Identification of [3H] histamine binding sites on gastric mucosal cells unrelated to histamine H2-receptors

doi:10.1016/0006-291X(82)92093-9

Biochemical and Biophysical Research Communications

Volume 108, Issue 3, 15 October 1982, Pages 965-969

https://doi.org/10.1016/0006-291X(82)92093-9 Get rights and content

Abstract

Binding of ³H-histamine to guinea pig gastric mucosal cells was inhibited by various imidazole and indole derivatives as well as by histamine and its H₂-receptor agonists and antagonists. In contrast to the H₂-agonists or H₂-antagonists, these derivatives (e.g. imidazole, 4-hydroxymethyl imidazole, tryptamine, serotonin), neither increased cellular cyclic AMP nor altered the increase in cyclic AMP caused by histamine. The imidazole derivatives were more potent in inhibiting [³H]histamine binding than the corresponding indole derivatives. These results confirm our earlier observations suggesting that gastric cells posses a class of binding sites for ³H-histamine that is not linked to adenylate cyclase and is unrelated to the histamine H₂-receptor.

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Cited by (6)

Solubilization and characterization of a low-affinity histamine-binding site on human blood mononuclear cells
1986, Molecular Immunology
The extract of human peripheral blood lymphocytes and monocytes treated with Triton X-100, in direct- and competitive-binding studies, with 10⁻⁶−10⁻² M [¹⁴C]histamine contained a low-affinity binding site whose dissociation constant (K_d 1.8 × 10⁻⁴ M) was commensurate with the concns of histamine (10⁻⁶−10⁻³ M) that result from mast cell and basophil degranulation. Binding was enhanced by millimolar concns of divalent cations and by raising the incubation temp from 4 to 37°C. It was inhibited by trypsin, EDTA, agents interacting with thiol groups, and by Triton X-100 concns greater than 0.2%. Thus a low-affinity histamine receptor that maintains its ligand-binding properties after solubilization from the cell surface was identified.
Role of histamine in the cell turnover changes associated with experimental gastric ulceration in the mastomys
1985, Gastroenterology
Using an animal model of gastric ulceration, in vivo and in vitro methods were developed to assess the importance of histamine in the cell turnover abnormalities previously found to occur in the preulcerous phase of gastric ulceration induced by mucosal anaphylaxis, and by using specific H_1⁻ and H_2⁻ receptor agonists and antagonists to define which receptors were involved. In ovalbumin-immunized animals, intramucosal ovalbumin injection led to a highly significant increase in cell turnover as measured by [³H]thymidine uptake (p < 0.001). This increase was not affected by treatment with the H₂ antagonist cimetidine, but was significantly reduced by the H₁ antagonists promethazine and clemastine (p < 0.01). A cell culture method was then used to examine the effects of added histamine and its antagonists. Histamine at a concentration of 10⁻⁷ M was found to have a significant stimulatory effect on cell proliferation (p < 0.001), and this effect was blocked by promethazine and clemastine but not by cimetidine. In contrast, histamine at a concentration of 10⁻² M had an inhibitory effect on cell proliferation which was accentuated by cimetidine and partially reversed by promethazine and clemastine. The H₁ agonist betahistine was found to have stimulatory effects similar to those of histamine in low concentration (10⁻⁷ M and 10⁻⁶ M), but the H₂ agonist 4-methyl histamine did not affect thymidine uptake at these concentrations. Both H₁ and H₂ agonists had a similar inhibitory effect at a concentration of 10⁻² M. It is concluded that histamine probably plays an important part in the changes in cell kinetics associated with gastric ulceration induced by this method, and that the trophic effects of histamine are mediated by H₁-receptors. H₂-receptors appear to have only a limited role in the control of cell proliferation.
Action of ebrotidine, ranitidine and cimetidine on the specific binding to histamine H<inf>1</inf>- and H<inf>2</inf>-receptors
1997, Arzneimittel-Forschung/Drug Research
Histaminergic transmission in the mammalian brain
1991, Physiological Reviews
The preparation and characterization of [3H] histamine.2HCl at high specific activity1
1987, Journal of Labelled Compounds and Radiopharmaceuticals
Specific binding of 3H-tiotidine to histamine H<inf>2</inf> receptors in guinea pig cerebral cortex
1983, Nature

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Biochemical and Biophysical Research Communications

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References (12)

Biochem. Pharmacol

Biochim. Biophys. Acta

Biochim. Biophys. Acta

Biochim. Biophys. Acta

Mol. Pharmacol

Mol. Pharmacol

Cited by (6)

Solubilization and characterization of a low-affinity histamine-binding site on human blood mononuclear cells

Role of histamine in the cell turnover changes associated with experimental gastric ulceration in the mastomys

Action of ebrotidine, ranitidine and cimetidine on the specific binding to histamine H<inf>1</inf>- and H<inf>2</inf>-receptors

Histaminergic transmission in the mammalian brain

The preparation and characterization of [<sup>3</sup>H] histamine.2HCl at high specific activity<sup>1</sup>

Specific binding of <sup>3</sup>H-tiotidine to histamine H<inf>2</inf> receptors in guinea pig cerebral cortex